http://hdl.handle.net/20.500.12128/566
Tytuł: | Investigation of the biological properties of (hetero)aromatic thiosemicarbazones |
Autor: | Serda, Maciej Mrozek-Wilczkiewicz, Anna Jampilek, Josef Pesko, Matus Kralova, Katarina Vejsova, Marcela Musioł, Robert Ratuszna, Alicja Polański, Jarosław |
Słowa kluczowe: | Thiosemicarbazones; Iron chelators; In Vitro Anticancer Activity; Lipophilicity; Spinach Chloroplasts |
Data wydania: | 2012 |
Źródło: | Molecules, (2012), vol. 17, no. 11, p. 13483-13502 |
Abstrakt: | Two series of thiosemicarbazone-based iron chelators (twenty-seven compounds) were designed and synthesized using a microwave-assisted approach. Quinoline and halogenated phenyl were selected as parent scaffolds on the basis of a similarity search. The lipophilicity of the synthesized compounds was measured using HPLC and then calculated. Primary in vitro screening of the synthesized compounds was performed against eight pathogenic fungal strains. Only a few compounds showed moderate activity against fungi, and (E)-2-(quinolin-2-ylvinyl)-N,N-dimethylhydrazine-carbothioamide appeared to be more effective than fluconazole against most of the fungal strains tested. Antiproliferative activity was measured using a human colon cancer cell line (HCT-116). Several of the tested compounds showed submicromolar antiproliferative activity. Compounds were also tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. The structure-activity relationships are discussed for all of the compounds. |
URI: | http://hdl.handle.net/20.500.12128/566 |
DOI: | 10.3390/molecules171113483 |
ISSN: | 1420-3049 |
Pojawia się w kolekcji: | Artykuły (WNŚiT) |
Plik | Opis | Rozmiar | Format | |
---|---|---|---|---|
Serda_Investigation_of_the_biological_properties_of_heteroaromatic.pdf | 442,81 kB | Adobe PDF | Przejrzyj / Otwórz |
Uznanie Autorstwa 3.0 Polska Creative Commons